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HRID 1888809作成日:2026年10月27日

Sodium Acetate → 5-(2-Amino-thiazol-4-yl)-6-methyl-2-oxo-1-(3-trifluoromethyl-phenyl)-1,2-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide

https://huagongshe.com/reaction/1888809

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium AcetateHCID 517045—
反応物ThioureaHCID 2723790—
反応物5-(bromoacetyl)-6-methyl-N-[4-(methylsulfonyl)benzyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamideHCID 86614780—
溶媒EthanolHCID 702—
生成物5-(2-Amino-thiazol-4-yl)-6-methyl-2-oxo-1-(3-trifluoromethyl-phenyl)-1,2-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamideHCID 8661478169%

反応条件

温度90 °C

反応手順

5-Bromoacetyl-6-methyl-2-oxo-1-(3-trifluoromethyl-phenyl)-1,2-dihydro-pyridine-3-carboxylic acid 4-methanesulfonyl-benzylamide (Example 50 (c), 0.04 g, 0.067 mmol), thiourea (0.0067 g, 0.086 mmol), NaOAc (0.011 g, 0.136 mmol), EtOH (2 ml) and a magnetic stirrer bar were placed in a tube designed for microwave synthesis. The vial was sealed and the mixture was heated in a CEM Discover Microwave apparatus (100 W, 90° C.) for 20 minutes, giving complete conversion of the starting material to a single product according to LC-MS. The solvents were evaporated to give a crude mixture which was purified on preparative HPLC giving the title compound (0.026 g, 66%) as a slightly yellowish solid after freeze-drying the pure fractions.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08501784B2
出典データセットuspto-grants-2013_08
ORD IDord-1b3fe496dde14a2dab76905d463a6b62
出典メモuspto-grants-2013_08